EVP-6124

Short Summary : NAChRs agonist

Category : Neuroscience|Nicotinic Receptor

Purity : 0.98

CAS Number : 550999-75-2

Formula : C16H17ClN2OS

Molecular Weight : 320.84

SMILE : O=C(C1=CC2=C(C(Cl)=CC=C2)S1)NC(C3)C4CCN3CC4

Solubility : DMSO

Storage : Store at -20°C

Description : EVP-6124 is a partial agonist of 7 neuronal nicotinic acetylcholine receptors (nAChRs) that was proved high-affinity in vitro and in vivo. [1]
EVP-6124 was proved to show selectivity for 7 but low-affinity of 42 nAChRs in some binding and functional experiments. EVP-6124 had good brain penetration and an adequate exposure time. [1,2]
Co-administration of EVP-6124 and the selective nAChRs antagonist could contribute to the release of DA, ACH, and Glu. This could be used to treat cognitive impairment and possibly other dimensions of psychopathology. Co-administration of donepezil at 0.1 mg/kg, p.o. and EVP-6124 at 0.03 mg/kg proved to be fully restored memory while each of these did not improve memory in this task. [1] Pretreatment with the selective 7 nAChR antagonist, methyllycaconitine (MLA, 1.0 mg/kg), significantly blocked cortical DA and Glu efflux induced by EVP-6124 (0.1 mg/kg). [2,3]
References:1. Jos Prickaerts, Nick P. van Goethem, et al. EVP-6124, a novel and selective 7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of 7 nicotinic acetylcholine receptors. Neuropharmacology, 2012,62 (2): 1099-1110. 2. Mei Huang, Anna R. Felix, et al. Chaya Bhuvaneswaran, Dana Hilt, Gerhard K nig, Herbert Y. Meltzer, The alpha-7 receptor agonist EVP-6124 increases dopamine and glutamate efflux in rat medial prefrontal cortex and nucleus accumbens. Biochemical Pharmacology, 2011, 82 (8): 1040. 3. Mei Huang, Anna R. Felix, et al. The novel 7 nicotinic acetylcholine receptor agonist EVP-6124 enhances dopamine, acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens. Psychopharmacology, 2014, 231:4541-4551.

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